The new antihypertensive I1-receptor agonist (4) was rationally synthetized by the insertion of a phenyl group in the ortho position of the aromatic ring of the I1-selective antagonist (3). This "antagonismagonism" modulation, highlights the existence of expected analogies between I1- and α2-adrenoreceptor systems. Chirality proves to be crucial for the activation of I1-receptors, since the cardiovascular effects are produced exclusively by the (S)-(+)-4 enantiomer.
Keywords: Antihypertensive activity, I1-ligands, antagonism/agonism, molecular superposition
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